Aurora A Inhibitor I (TC-S 7010)

For research use only.

Catalog No.S1451

21 publications

Aurora A Inhibitor I (TC-S 7010) Chemical Structure

Molecular Weight(MW): 588.07

Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B.

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10mM (1mL in DMSO) USD 280 In stock
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Selleck's Aurora A Inhibitor I (TC-S 7010) has been cited by 21 publications

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Biological Activity

Description Aurora A Inhibitor I is a novel, potent, and selective inhibitor of Aurora A with IC50 of 3.4 nM in a cell-free assay. It is 1000-fold more selective for Aurora A than Aurora B.
Features Aurora A Inhibitor I is a novel, potent, and selective inhibitor to Aurora A.
Targets
Aurora A [1]
(Cell-free assay)
3.4 nM
In vitro

Aurora A Inhibitor I is a 2,4-dianilinopyrimidine that selectively and potently inhibits Aurora A. Aurora A Inhibitor I effectively inhibits the proliferation of HCT116 and HT29 cells, with IC50 of 190 nM and 2.9 μM, respectively. The Aurora A selectivity of Aurora A Inhibitor I against Aurora B depends on a single amino acid (Thr217) of Aurora A. [1] In KCL-22 cells, Aurora A Inhibitor I (1-5 μM) increases G2/M cell fraction, induces histone H3 serine 10 phosphorylation, and suppresses mitotic Aurora A autophosphorylation on Thr288. Aurora A Inhibitor I (0.5-5 μM) also suppresses cell proliferation in KCL-22 cells, as well as BCR-ABL-negative leukemia cell lines KG-1 and HL-60. Aurora A Inhibitor I effectively induces apoptosis in KCL-22 cells at 5 μM. [2] In a recent study, Aurora A Inhibitor I is also found to inhibit cell growth of HCT116, HT29, and HeLa cells, with IC50 of 377.6 nM, 5.6 μM, and 416 nM. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 cells MkLkVJJwdGmoZYLheIlwdiCjc4PhfS=> MX20JIRigXN? NFjtdJNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC0JIRigXNiYomgZ4VtdHSrdHXyJIF{e2G7LDDJR|UxRTBwMUmg{txO MYWxPVQxOjZ|Mx?=
HT-29 cells M1WyRnBzd2yrZnXyZZRqd25iYYPzZZk> Ml3JOEBl[Xm| MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHHmeIVzKDRiZHH5d{BjgSClZXzseIl1\XJiYYPzZZktKEmFNUC9Nk46KM7:TR?= NYfV[5k3OTl2MEK2N|M>

... Click to View More Cell Line Experimental Data

Protocol

Kinase Assay:

[1]

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Auroras A and B Inhibition Assays:

Both Auroras A and B are assayed in ELISA format using a GST fusion (pGEX-4T) of the N-terminus of Histone H3 (aa 1−18) as substrate. Plates are coated with 2 μg/mL substrate in PBS then blocked with 1 mg/mL I-block in PBS. Kinase reactions are run for 40 min with 5 ng/mL (0.16 nM) Aurora A or 45 ng/mL (1.1 nM) Aurora B at 30 μM ATP (~ Km) in kinase buffer. Final DMSO concentration is 4%. Product is detected by incubation with antiphosphohistone H3 (Ser10) 6G3 mouse monoclonal antibody and sheep-anti-mouse HRP conjugate, followed by washing and addition of TMB substrate. After quenching with 1 M phosphoric acid, plates are read at 450 nM.
Cell Research:

[1]

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  • Cell lines: HCT116 and HT29 cells
  • Concentrations: 0.1 nM - 10 μM, dissolved in medium lacking serum and glutamine (dissolved in DMSO as stock solution)
  • Incubation Time: 72 hours
  • Method:

    Cells are seeded in 384-well plates on day 0 in 50 μL of complete medium and incubated overnight in a 5% CO2 atmosphere at 37 °C. On day 1, 10 μL of Aurora A Inhibitor I is added. On day 4, plates are allowed to reach room temperature, and 30 μL Cell Titer-Glo reagent is added to each well to measure total ATP levels. Plates are read after shaking 15 min at room temperature.


    (Only for Reference)
Animal Research:

[5]

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  • Animal Models: BALB/c nude mice bearing ARID1A isogenic tumors
  • Dosages: 30 and 60 mg/kg
  • Administration: IP
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 118 mg/mL (200.65 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5%DMSO+40%PEG300+5%Tween80+50%ddH2O
For best results, use promptly after mixing.
1.25mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 588.07
Formula

C31H31ClFN7O2

CAS No. 1158838-45-9
Storage powder
in solvent
Synonyms N/A
Smiles CCN1CCN(CC1)C(=O)CC2=CC=C(NC3=NC(=C(F)C=N3)NC4=CC=C(C=C4)C(=O)NC5=CC=CC=C5Cl)C=C2

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID